Solid dispersions of the three drugs in hydroxy propylmethylcellulose hpmc, with drug. A modified solvent method for preparation of solid dispersions. Because solid dispersions are in a metastable state and thus are a state function of the processing, they are strongly impacted by the manufacturing process. The concept of solid dispersion was firstly introduced by sekiguchi and obi10, 2. The formulation of drugs having low aqueous solubility using solid dispersion method has been an active area of research since 1960. Research article enhancement of solubility and dissolution rate of irbesartan by solid dispersion technique g. The release of domperidone was decreased in the solid dispersion with eudragit rlpo. Solid dispersions were prepared by solvent evaporation. Chaitanya 1department ofpharmaceutics,bharatinstitute technologypharmacy,ibrahimpatnam, hyderabad,andhrapradesh,india. Fusion method melt method 7, 8, 1011 the accurately weighed amount of carrier was melted in a porcelain dish and calculated amount of mebendazole was added with thorough mixing for 12 minutes followed by quick cooling. Solid dispersions have attracted considerable interest as an efficient means of improving the. A solid dispersion generally composed of two components the drug and the polymer matrix. Enhancement of oral bioavailability and solid dispersion.
A modified solvent method for preparation of solid dispersions sanjay j. The solid dispersion is based on the concept that the drug is dispersed in an inert watersoluble carrier at solid state. Solid dispersions were prepared by solvent evaporation method. Among them, solid dispersion is promising technologies to improve dissolution which is defined as the dispersion of active ingredient in an inert carrier in solid state. Solid dispersions have attracted considerable interest as an efficient means of improving the dissolution rate and hence the bioavailability of a range of hydrophobic drugs. The release rate of carvedilol from solid dispersions was determined using united states pharmacopeia usp dissolution testing apparatus 2 paddle method. Recently, solid dispersion is one of the most widely used and successful techniques in formulation development. Abstract the aim of the study was to improve the solubility and dissolution rate of the drug verapamil hcl using solid dispersion sustained release matrix tablets by direct compression method. Processing impact on performance of solid dispersions. Improving the chemical stability of amorphous solid. Solid dispersion is one of the most promising approaches for solubility enhancement. Water solubility enhancement of atorvastatin by solid dispersion method. Formulation and evaluation of solid dispersions of. Solid dispersion technique for improving solubility of some poorly.
Solubility enhancement of diacerein by solid dispersion. Solid dispersion, co poloxamer the study was designed to formulate novel spironolactone, a bcs class ii drug loaded solid dispersion system sds with improved dissolution rate. Fundamental aspects of solid dispersion technology for poorly. Formulation and evaluation of ritonavir solid dispersions.
The term solid dispersion refers to the dispersion of one or more active ingredients in a. Solid dispersion also termed as coprecipitates and melts. Solid dispersion sd is one of such methods and it involves a dispersion of one or more active ingredients in an inner carrier or matrix in solid state prepared by melting, dissolution in solvent or meltingsolvent method4. The promising results of the prepared binary systems open the avenue for further oral formulation of stp.
Solid dispersion is one of the techniques used to increase the dissolution rate of the lipophilic drugs. Pharmaceutical applications of solid dispersion systems. Three solid dispersion preparation techniques are typically employed. The resulting mixture is called a solid dispersion. Fundamental aspects of solid dispersion technology for. Product name, api, polymer, maximum api dose per tablet or capsule mg, api tm c, solid dispersion preparation method, year of approval. The solid dispersion may optionally be encapsulated in hard gelatin capsules, compressed into a tablet, or may be granulated with a pharmaceutically acceptable granulating agent. Kshirsagar, anand ubhe, jasmine malshe, vidula sengaokar a. In particular, the processing route may control properties of solid dispersions, such as particle attributes. Carbamazepine cbznicotinamide nic cocrystal solid dispersions were prepared with polymer carriers pvpva. The invention discloses a posaconazole solid dispersion which is composed of posaconazole and a watersoluble polymer according to a weight ratio of 1. Solid dispersion is one of these methods, which was most widely and successfully applied to improve the solubility, dissolution rates and consequently the bioavailability of poorly soluble drugs. The different types of solid dispersions based on their molecular arrangement have been highlighted. Applications of solid dispersions pharmaceutical research.
Different formulation strategies have been taken to prepare solid dispersions. Solid dispersion, pioglitazone hcl, eudragit epo, peg 6000 introduction recently many potential drug candidates have been. The technique has been used for a wide variety of poorly aqueous soluble drug. According to this method, a drug is thoroughly dispersed in a watersoluble carrier by suitable method of preparation. Dispersion methods of preparation of colloids, chemistry. Although these are also widely recommended as preparative methods for phase diagram determination, few examples exist concerning their effect on the resulting. Solid dispersion a novel approach for enhancement of bioavailability of poorly soluble drugs in oral drug. Several methods such as solid dispersion, complexation, lipidbased systems, micronization, nanonization, and cocrystals were developed to improve the solubility of hydrophobic drugs. In these methods, larger particles of a substance suspensions are broken into smaller particles. Solid dispersions of poorly watersoluble drugs with watersoluble carriers reduce the incidence of these problems and enhanced dissolution.
In this study, various hydrophilic polymers such as pvp k17, pvp k30, and hpmc e3 were used to prepare pioglitazone solid dispersion by the spray drying method. The invention belongs to the technical field of pharmacy, and specifically relates to a posaconazole solid dispersion and a preparation method thereof. Overview of the manufacturing methods of solid dispersion. Pdf water solubility enhancement of atorvastatin by. Solid dispersion of furosemide in ssg was prepared in ratios of 1. Different methods used in solid dispersion iosr journal of. The solid dispersion showing better release profile was chosen to formulate into a tablet dosage form of weight 600 mg. In each case, the solid dispersion was characterized by fourier transform infrared ftir spectroscopy, differential scanning calorimetry dsc, and xray diffraction xrd to. Preparation and evaluation of solid dispersion tablets by. Alternatively, the sample may also be prepared by conventional methods melt extrusion, spray drying, and coprecipitation and then annealed at suitable temperature to generate drug crystals in situ 14. The aim of this study was to establish a new preparation method for solid dispersion formulation sdf of tacrolimus, a poorly watersoluble drug, without dichloromethane, because no use of dichloromethane is recommended by ich harmonized tripartite guideline. Solid dispersion technique has been extensively used to increase the solubility of a poorly watersoluble drug. Solid dispersion approach improving dissolution rate of stiripentol.
Solid dispersion as a dosage form has been established a superior option for the drugs having poor aqueous solubility. The melting method has also been used to improve solubility of poorly. It characteristics of drugs they increase the oral bioavailability. The term solid dispersion refers to a group of solid products consisting of at least two different components, generally a hydrophilic matrix and a hydrophobic drug. Preparation and characterization of solid dispersions of carvedilol. The technique of solid dispersion and solid solution is used to influence drug absorption and its subsequent bioavailability through increased dissolution rate. Solid dispersion, technology is the science of dispersing one or more active ingredient in a carrier or matrix at solid state for improving dissolution of poorly watersoluble drugs for. Formulation, physicochemical evaluation, and dissolution.
The solid dispersions as a dispersion of one or more active ingredients in an inert carrier or matrix. In this method, the solid dispersion is prepared by intimate mixing of drug crystals and polymer via cryogenic milling. Solid dispersion is defined as dispersion of one or more active ingredients hydrophobic in an inert carrier hydrophillic at solid state prepared by melting fusion method, solvent, or melting solvent method. Solid dispersion is defined as a dispersion of one or more active ingredients in an inert carrier or matrix of solid state prepared by melting fusion, solvent or melting solvent method. Fusion method is the oldest method used for the preparation of solid dispersions as the first solid dispersion created for pharmaceutical application were prepared by the fusion method. Pioglitazone solid dispersion system prepared by spray.
From the results, it was clear that solid dispersion formulation showed improved dissolution rate than pure drug and physical mixture. Also disclosed are methods of making said solid dispersion and methods of treating an hiv infection employing said solid dispersion. It is also referred as the melt method only when the starting materials are in crystalline state. For this purpose binary and ternary solid dispersion were prepared by co precipitation method using poloxamer 407 only and mixture of poloxamer 407 with a. Solid dispersion technique for improving solubility of.
Thermodynamic phase behavior of apipolymer solid dispersions. In this work, the phase behaviors of solid dispersions were investigated as a function of the api as well as of the type and molecular weight of the carrier polymer. Fusion method was used for the preparation of solid dispersions. Therefore increase in dissolution of poorly soluble drugs by solid dispersion technique presents a challenge to the formulation scientists. Solid dispersion can be prepared by various methods such as solvent evaporation and melting method. The term solid dispersion refers to the dispersion of one or more active ingredients in a hydrophilic inert carrier matrix at molecular level. Formulation and evaluation of solid dispersions of an. Solid dispersion sd is one of such methods and encloses a dispersion of one or more active component in an inert carrier or matrix in the solid state organized by melting, dissolution in a solvent or meltingsolvent method 2,11. Solid dispersion a novel approach for enhancement of. Solid dispersion as an approach for bioavailability. Applications of solid dispersions bindu yadav 1 and y. When the solid dispersion comes in contact with the aqueous medium, the inert carrier dissolves. To improve the bioavailability of poorly soluble active pharmaceutical ingredients apis, these materials are often integrated into a polymer matrix that acts as a carrier. Formulation, physicochemical evaluation, and dissolution studies of carbamazepine solid dispersions m.
Solid dispersion formulations of pioglitazone hcl using. Preparation and characterization of solid dispersions of. Among several methods, solid dispersion has attracted attention of the researchers for previous 50 years. One advantage of the direct mixing method is being able to avoid complications of. Solid solutions and dispersions are generally made by the melt method or the solution. The formulation of drugs having low aqueous solubility using solid. Solid dispersion are prepared by the physical triturating, solvent evaporation, fusion method. Razia begum department of pharmaceutical technology, shri vishnu college of pharmacy, vishnupur, bhimavaram534202, ap, india. To study the evolution parameter of solid dispersion. The drug can be dispersed molecularly, in amorphous particles clusters or in. It is simple, scalable, convenient method and prepared using numerous processes 3. Solid dispersions embed active pharmaceutical ingredients in polymeric carriers to improve their solubility. Numerous methods are existing to prepare the solid dispersions such as melting method, solvent evaporation method, fusion method, kneading.
Some of the practical aspects to be considered for the preparation of. The mechanisms of increased dissolution rates of drugs, solid dispersed in polyvinylpyrrolidone carriers. Solid dispersion technique for improving solubility of some poorly soluble drugs mogal s. The solubility and dissolution rates of oxcarbazepine and quetiapine were. The term solid dispersion refers to a grou p of solid products consisting of at least two differe nt components, generally a hydrophilic matrix and a hydrophobic drug. Solid solutions and dispersions are used in many routes of drug administration, such as oral, mucosal vaginal, rectal, buccal, ocular, subcutaneous, subdermal, and transdermal, and can help alleviate some of these issues. The objective of the current work was to improve aqueous solubility of pioglitazone by the solid dispersion approach using the spray drying technique. Solid dispersions in watersoluble carriers have engrossed considerable interest as a means of improving the dissolution rate and bioavailability of hydrophobic drugs. The solid dispersion technique with pvp k30 as a carrier provides a promising way to. Solid dispersion as an approach for bioavailability enhancement of. To explore insitu forming cocrystal as a singlestep, efficient method to significantly depress the processing temperature and thus minimize the thermal degradation of heatsensitive drug in preparation of solid dispersions by melting method mm and hot melt extrusion hme.
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